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    Pharmaceuticals containing prostaglandin I.sub.2
    4.
    发明授权
    Pharmaceuticals containing prostaglandin I.sub.2 失效
    含有前列腺素I2的药物

    公开(公告)号：US4699921A

    公开(公告)日：1987-10-13

    申请号：US763618

    申请日：1985-08-08

    申请人： Masakatsu Shibasaki ,  Mikiko Sodeoka ,  Yuji Ogawa ,  Toshiaki Mase ,  Akira Ishibashi ,  Daijiro Horii ,  Toshiji Kanayama ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Ishiyama ,  Yoshio Hayashi

    发明人： Masakatsu Shibasaki ,  Mikiko Sodeoka ,  Yuji Ogawa ,  Toshiaki Mase ,  Akira Ishibashi ,  Daijiro Horii ,  Toshiji Kanayama ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Ishiyama ,  Yoshio Hayashi

    IPC分类号： C07C59/46 ,  A61K31/557 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/12 ,  C07C51/00 ,  C07C67/00 ,  C07C69/732 ,  C07C405/00

    CPC分类号： C07C405/0083 ,  A61K31/557 ,  Y02P20/55

    摘要： Disclosed is a pharmaceutical composition having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group, A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or a 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof; the asymmetric center in the substituent represented by A is in the R-configuration or the S-configuration or a mixture thereof.Pharmaceutical compositions containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.

    摘要翻译： 本发明公开了一种具有循环改善作用和抗溃疡效果的药物组合物，其含有下述式表示的前列腺素I 2类似物或其无毒性盐或环糊精包合物作为有效成分：其中R 1表示氢原子， 碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基，A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2 1-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1-二甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基 -3-戊炔基或2,6-二甲基-5-庚烯基; 4-和5-位的碳原子之间的双键是E或Z或它们的混合物; 由A表示的取代基中的不对称中心是R构型或S-构型或其混合物。 含有本发明的前列腺素I2类似物作为活性成分的药物组合物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

    Pharmaceuticals containing prostaglandin I.sub.2
    8.
    发明授权
    Pharmaceuticals containing prostaglandin I.sub.2 失效
    含有前列腺素I2的药物

    公开(公告)号：US5053526A

    公开(公告)日：1991-10-01

    申请号：US511945

    申请日：1990-04-16

    申请人： Masakatsu Shibasaki ,  Mikiko Sodeoka ,  Yuji Ogawa ,  Toshiaki Mase ,  Akira Ishibashi ,  Daijiro Horii ,  Toshiji Kanayama ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Ishiyama ,  Yoshio Hayashi

    发明人： Masakatsu Shibasaki ,  Mikiko Sodeoka ,  Yuji Ogawa ,  Toshiaki Mase ,  Akira Ishibashi ,  Daijiro Horii ,  Toshiji Kanayama ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Ishiyama ,  Yoshio Hayashi

    IPC分类号： A61K31/557 ,  C07C405/00

    CPC分类号： C07C405/0083 ,  A61K31/557

    摘要： Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt of its salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group; A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or 1 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof, the asymmetric center in the substituent represented by A is R-configuration or S-configuration or a mixture thereof.The pharmaceuticals containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.

    摘要翻译： 本发明公开了一种具有循环改善作用和抗溃疡效果的药物，其含有下述式表示的前列腺素I2类似物或其盐的无毒性盐或其环糊精包合物作为有效成分：其中R1表示氢 原子，碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基; A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1 2-甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基-3-戊炔基或1,6-二甲基-5-庚烯基; 在4-和5-位碳原子之间的双键是E或Z或其混合物，由A表示的取代基中的不对称中心是R-构型或S-构型或其混合物。 含有本发明的前列腺素I2类似物作为活性成分的药物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

    Prophylactic and therapeutic composition for circulatory disorders and method of treatment
    9.
    发明授权
    Prophylactic and therapeutic composition for circulatory disorders and method of treatment 失效
    循环障碍的预防和治疗组合物及治疗方法

    公开(公告)号：US4857542A

    公开(公告)日：1989-08-15

    申请号：US122516

    申请日：1987-11-19

    申请人： Hiroyoshi Nishi ,  Toshiaki Watanabe ,  Satoshi Yuki ,  Yasuhiro Morinaka ,  Katsuhiko Iseki ,  Hiroko Sakurai

    发明人： Hiroyoshi Nishi ,  Toshiaki Watanabe ,  Satoshi Yuki ,  Yasuhiro Morinaka ,  Katsuhiko Iseki ,  Hiroko Sakurai

    IPC分类号： C07D231/20 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D231/56

    CPC分类号： C07D231/56 ,  C07D231/20 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28

    摘要： A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms; or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 5 to 7 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, a benzyl group, a naphthyl group, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are the same or different selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, hydroxyalkyl groups having 1 to 3 carbon atoms, alkoxycarbonyl groups having total carbon number of 2 to 5, alkylmercapto groups having 1 to 3 carbon atoms, alkylamino groups having 1 to 4 carbon atoms, dialkylamino groups having total carbon number of 2 to 8, halogen atoms, trifluoromethyl group, carboxyl group, cyano group, hydroxyl group, nitro group, amino group and acetamide group,or a pharmaceutically acceptable salt thereof as an acitve ingredient.The agent of the present invention is useful as a prophylactic and therapeutic agent for circulatory disorders, particularly as an inhibitor agaisnt lipid peroxidation and/or an agent for normalizing cerebral dysfunctions.

    摘要翻译： 一种循环系统疾病的预防和治疗剂，其包含下式的吡唑啉酮衍生物：其中R 1表示氢原子，芳基，具有1至5个碳原子的烷基或具有总碳数的烷氧基羰基烷基 3至6; R2表示氢原子，芳氧基，芳基巯基，碳原子数1〜5的烷基或碳原子数1〜3的羟烷基。 或R 1和R 2一起表示具有3至5个碳原子的亚烷基; R3表示氢原子，碳原子数1〜5的烷基，碳原子数5〜7的环烷基，碳原子数1〜3的羟烷基，苄基，萘基或苯基， 未取代或被1〜3个选自碳原子数1〜5的烷基，碳原子数为1〜5的烷氧基，碳原子数1〜3的烷氧基，碳原子数1〜3的烷氧基，烷氧基羰基， 总碳数为2至5，具有1至3个碳原子的烷基巯基，具有1至4个碳原子的烷基氨基，总碳数为2至8的二烷基氨基，卤素原子，三氟甲基，羧基，氰基，羟基 基团，硝基，氨基和乙酰胺基，或其药学上可接受的盐作为acitve成分。 本发明的药剂可用作循环障碍的预防和治疗剂，特别是作为抑制剂脂质过氧化作用的抑制剂和/或用于使脑功能障碍正常化的药剂。

    (2-chloro-3-oxo-1-alkenyl)bicyclo(3.3.0)octane derivative
    10.
    发明授权
    (2-chloro-3-oxo-1-alkenyl)bicyclo(3.3.0)octane derivative 失效
    （2-氯-3-氧代-1-烯基）双环（3.3.0）辛烷衍生物

    公开(公告)号：US4810805A

    公开(公告)日：1989-03-07

    申请号：US943484

    申请日：1986-12-19

    申请人： Masakatsu Shibasaki ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Aoki ,  Yoshio Hayashi

    发明人： Masakatsu Shibasaki ,  Katsuhiko Iseki ,  Masaki Shinoda ,  Chiyoko Aoki ,  Yoshio Hayashi

    IPC分类号： C07F9/38 ,  C07C67/343 ,  C07C69/738 ,  C07C405/00 ,  C07F9/40 ,  C07D309/12

    CPC分类号： C07C405/0083

    摘要： There are disclosed a (2-chloro-3-oxo-1-alkenyl)-bicyclo[3.3.0 octene derivative represented by the formula: ##STR1## wherein R.sup.1 represents --CH.sub.2 CH.sub.2 CH.sub.2 COOR.sup.5, --CH.sub.2 CH.sub.2 --O--CH.sub.2 COOR.sup.5, --CH.dbd.CHCH.sub.2 COOR.sup.5 or --CH.sub.2 CH.sub.2 C.tbd.C--COOR.sup.5 group where R.sup.5 in the groups represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, an acyl group having 1 to 7 carbon atoms, a tri(1 to 7 carbon atoms)-hydrocarbylsilyl group or a group forming an acetal bonding with an oxygen atom of a hydroxy group; R.sup.3 represents a straight or branched alkyl group having 3 to 10 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms, which may be substituted by at least one alkyl group having 1 to 4 carbon atoms, a straight or branched alkenyl group having 3 to 12 carbom atoms, a straight or branched alkynyl group having 3 to 8 carbon atoms, a phenyl group or a phenoxy group which may have substituents, an alkoxy group having 1 to 6 carbon atoms or an alkyl group substituted by a cycloalkyl group having 5 to 8 carbon atoms, and a process for preparing the same which comprises reacting an aldehyde represented by the formula: ##STR2## wherein R.sup.1 and R.sup.2 have the same meanings as defined above, with kotophosphonate represented by the formula: ##STR3## wherein R.sup.3 has the same meaning as defined above and R.sup.4 represents an alkyl group having 1 to 10 carbon atoms, in the presence of a base.

    摘要翻译： 公开了由下式表示的（2-氯-3-氧代-1-烯基） - 二环[3.3.0辛烯衍生物：其中R 1表示-CH 2 CH 2 CH 2 COOR 5，-CH 2 CH 2 -O-CH 2 COOR 5，-CH = CHCH 2 COOR 5 或-CH 2 CH 2 C 3 CON COROR 5基团，其中基团中的R 5表示氢原子或具有1至6个碳原子的烷基; R2表示氢原子，碳原子数1〜7的酰基，三（1〜7个碳原子） - 烃基甲硅烷基或与羟基形成缩醛键的基团。 R3表示可以被至少一个具有1至4个碳原子的烷基取代的具有3至10个碳原子的直链或支链烷基，具有4至7个碳原子的环烷基，具有3个碳原子的直链或支链烯基 至12个碳原子，具有3至8个碳原子的直链或支链炔基，可具有取代基的苯基或苯氧基，具有1至6个碳原子的烷氧基或被具有5个环烷基的环烷基取代的烷基 至8个碳原子，及其制备方法，其包括使由下式表示的醛：其中R 1和R 2具有与上述相同的含义，与下式表示的焦磷酸酯反应：其中R 3具有 在碱的存在下，与上述定义相同，R 4表示具有1至10个碳原子的烷基。